文献类型：期刊文献

英文题名：Micelle controlled release of 5-fluorouracil: Follow the guideline for good polymer-drug compatibility

作者：Yuan, Ming[1];Xiao, Yan[1];Vanminh Le[2,3];Wei, Chao[1];Fu, Yutong[1];Liu, Jianwen[2,3];Lang, Meidong[1]

机构：[1]E China Univ Sci & Technol, Sch Mat Sci & Engn, Minist Educ, Key Lab Ultrafine Mat, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[3]E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2014

卷号：457

期号：1

起止页码：116

外文期刊名：COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS

收录：;EI(收录号：20142517853069);WOS:【SCI-EXPANDED(收录号:WOS:000340340600016)】；

基金：This research was supported by the National Natural Science Foundation of China (51103041, 21274039), the Natural Science Foundation of Shanghai (11ZR1409200), Basic Research Key Program Project of Science and Technology Commission of Shanghai Municipality (12JC1403000, 12JC1403100), Specialized Research Fund for the Doctoral Program of Higher Education (20130074110007), Key Subject of Shanghai Municipal Education Commission (J50102).

语种：英文

外文关键词：Poly(epsilon-carprolactone); 5-Fluorouracil; Polymer-drug compatibility; Flory-Huggins interaction parameter; Drug delivery system

摘要：Flory-Huggins interaction parameter (chi(pd)) was introduced to qualitatively evaluate the drug-polymer compatibility between hydrophilic 5-fluorouracil (5-FU) and hydrophobic core block, which was formed by poly[gamma-(carbamic acid benzyl ester)-epsilon-caprolactone] (PCABCL) and poly(epsilon-caprolactone) (PCL). The calculation results indicated that PCABCL had better affinity with 5-FU than PCL. Thus, a series of diblock polymers monomethoxy poly(ethylene glycol)-b-poly[-gamma-(carbamic acid benzyl ester)-epsilon-caprolactone] (mPEG(45)-b-PCABCL(n)) was synthesized, followed by the preparation of 5-FU loaded micelles. The introduction of gamma-(carbamic acid benzyl ester) (CAB) group significantly decreased the crystallinity of copolymers and increased the hydrophilicity of the micellar core, leading to an improved drug loading content. These micelles had high stability and spherical morphology. The release behavior could be turned by the length of core-forming block. Moreover, micelles prepared by mPEG(45)-b-PCABCL(19) displayed the highest 5-FU loading content and the most controlled release behavior. These blank micelles showed very low toxicity against HCT116 cancer cells. Meanwhile 5-FU loaded micelles exhibited a concentration dependent increase in HCT116 cell death by inducing cell apoptosis in vitro. These results indicated that these micelles have great potential in cancer therapy. (C) 2014 Elsevier B.V. All rights reserved.